2. Epigenetics
  3. Histone Methyltransferase
  4. SGC0946

SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells.

For research use only. We do not sell to patients.

SGC0946 Chemical Structure

SGC0946 Chemical Structure

CAS No. : 1561178-17-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 108 In-stock
Solution
10 mM * 1 mL in DMSO USD 108 In-stock
Solid
1 mg USD 37 In-stock
5 mg USD 79 In-stock
10 mg USD 139 In-stock
50 mg USD 320 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

SGC0946 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells[1][2][3].

IC50 & Target

DOT1L

.3 nM (IC50)

In Vitro

SGC0946 (0-100 μM; 4 days) inhibits DOT1L with IC50 of 2.65 nM in A431 cells[1].
? SGC0946 (1, 5 μM; 14 days) displays selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells (transformed with the MLL-AF9 fusion oncogene)[1].
? SGC0946 (1 μM; 3-7 days) shows time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation[1].
? SGC0946 (1 μM, 7 days) effectively inhibits MLL target genes, HOXA9 and Meis1[1].
? SGC0946 (0.2, 2, or 20 μM; 12 days) reduces proliferation and survival of ovarian cancer cells by inhibiting DOT1L enzymatic activity[2].
? SGC0946 (10 μM; 12 days) induces G1 phase arrest by blocking DOT1L in SK-OV-3 and TOV21G cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SGC0946 Related Antibodies

Cell Viability Assay[1]

Cell Line: A431 cells
Concentration: 0-100 µM
Incubation Time: 4 days
Result: Showed potent inhibitory activity against DOT1L with IC50 of 2.65 nM in A431 cells.

Cell Viability Assay[1]

Cell Line: Human cord blood cells (transformed with the MLL-AF9 fusion oncogene).
Concentration: 1, 5 µM
Incubation Time: 14 days
Result: Killed human cord blood cells transformed with an MLL-AF9 fusion oncogene.

Western Blot Analysis[1]

Cell Line: Molm13 MLL cells
Concentration: 1 µM
Incubation Time: 3-7 days
Result: Reduced H3K79me2 in Molm13 MLL cells in a time- and dose-dependent manner, and a complete inhibition exhibited at day 7.

Cell Proliferation Assay[2]

Cell Line: SK-OV-3 and TOV21G cells
Concentration: 0.2, 2, or 20 μM
Incubation Time: 12 days
Result: Inhibited the growth of both SK-OV-3 and TOV21G cells in a dose- and time-dependent manner.
Reduced the colony of both SK-OV-3 and TOV21G cells.

Cell Cycle Analysis[2]

Cell Line: SK-OV-3 and TOV21G cells
Concentration: 10 μM
Incubation Time: 12 days
Result: Induced increased G1 population and decreased S phase and G2/M phase cells in asynchronized SK-OV-3 and TOV21G cells.
In Vivo

SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD-SCID mice (4-week-old; mouse orthotopic xenograft ovarian cancer model)[2].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; twice a week for 6 weeks.
Result: Significantly suppressed growth of tumor (size and weight of tumor masses smaller than the untreated group).
Inhibited DOT1L enzymatic activity and decreased H3K79me2,CDK6, and cyclin D3 levels in the tumors.
Molecular Weight

618.57

Formula

C28H40BrN7O4
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

NC1=NC=NC2=C1C(Br)=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C)O3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (80.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6166 mL 8.0832 mL 16.1663 mL
5 mM 0.3233 mL 1.6166 mL 3.2333 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.68%

COA (251 KB) LCMS (120 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6166 mL 8.0832 mL 16.1663 mL 40.4158 mL
5 mM 0.3233 mL 1.6166 mL 3.2333 mL 8.0832 mL
10 mM 0.1617 mL 0.8083 mL 1.6166 mL 4.0416 mL
15 mM 0.1078 mL 0.5389 mL 1.0778 mL 2.6944 mL
20 mM 0.0808 mL 0.4042 mL 0.8083 mL 2.0208 mL
25 mM 0.0647 mL 0.3233 mL 0.6467 mL 1.6166 mL
30 mM 0.0539 mL 0.2694 mL 0.5389 mL 1.3472 mL
40 mM 0.0404 mL 0.2021 mL 0.4042 mL 1.0104 mL
50 mM 0.0323 mL 0.1617 mL 0.3233 mL 0.8083 mL
60 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6736 mL
80 mM 0.0202 mL 0.1010 mL 0.2021 mL 0.5052 mL
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SGC0946 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SGC09461561178-17-3SGC 0946SGC-0946Histone MethyltransferaseleukemiaMLL-rearrangeovarian cancerMolm13 MLLcord blood cellsSK-OV-3TOV21GInhibitorinhibitorinhibit

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